Etoposide freeze-dry powder preparation for injection and preparation method thereof

Abstract

The invention relates to the technical field of medicament and discloses an etoposide freeze-dried powder preparation used for injection, which is convenient to be used in clinic, is high in bioavailability, is low in cost and can cure solid tumors. The medicament can quickly achieve effective curing concentration in a body when being directly injected through vein or muscle; moreover, the first-pass effect of the medicament to a liver is reduced, the bioavailability of the medicament in the body is improved, and the freeze-dried powder preparation used for injection is more convenient to be transported and can be stored for a longer time. The etoposide freeze-dried powder preparation used for injection contains the etoposide or the pharmaceutically acceptable salt thereof and pharmaceutically acceptable accessories used as active components; wherein, the weight percentage of the etoposide or the pharmaceutically acceptable salt thereof can be 1 to 80 percent, preferably be 30 to 70 percent and more preferably be 40 to 60 percent; the content range thereof in the preparation is generally 1 to 1000mg and preferably be 10 to 500mg.

Description

technical field

[0001] The invention relates to the technical field of medicine, in particular to an etoposide freeze-dried powder injection preparation for injection that can treat solid tumors. Background of the Invention

[0002] Etoposide (4-desmethylepipodophyllotoxin-β-D-ethyl glucopyranoside) is a sugar metabolite of podophyllotoxin, a cell cycle specific antitumor drug with broad-spectrum anticancer activity , The commonly used clinical dosage forms are injections and oral soft capsules. Since etoposide is almost insoluble in water and has poor lipid solubility, the currently used clinical dosage forms have the disadvantage of low bioavailability to varying degrees. The glycoside is not easily soluble in water, and the existing injection is not very stable. Therefore, there is an urgent need to invent a stable, high bioavailability and low price etoposide lyophilized powder injection preparation for industrialized large-scale production to provide clinical needs. S...

Examples

Embodiment Construction

[0037] According to the above method, the following preparations of the present invention are prepared:

[0038] Formulation 1:

[0039] Etoposide or its pharmaceutically acceptable salt 50mg

[0040] Mannitol 150mg

[0041] Sodium bicarbonate amount

[0042] Formulation 2:

[0043] Etoposide or its pharmaceutically acceptable salt 100mg

[0044] Dextran 200mg

[0045] Sodium bicarbonate amount

[0046] Formulation 3:

[0047] Etoposide or its pharmaceutically acceptable salt 50mg

[0048] Glucose 200mg

[0049] Sodium bicarbonate amount

[0050] Formulation 4:

[0051] Etoposide or its pharmaceutically acceptable salt 50mg

[0052] Polyethylene Glycol 150mg

[0053] Sodium bicarbonate amount

technical field

[0001] The invention relates to the technical field of medicine, in particular to an etoposide freeze-dried powder injection preparation for injection that can treat solid tumors. Background of the Invention

[0002] Etoposide (4-desmethylepipodophyllotoxin-β-D-ethyl glucopyranoside) is a sugar metabolite of podophyllotoxin, a cell cycle specific antitumor drug with broad-spectrum anticancer activity , The commonly used clinical dosage forms are injections and oral soft capsules. Since etoposide is almost insoluble in water and has poor lipid solubility, the currently used clinical dosage forms have the disadvantage of low bioavailability to varying degrees. The glycoside is not easily soluble in water, and the existing injection is not very stable. Therefore, there is an urgent need to invent a stable, high bioavailability and low price etoposide lyophilized powder injection preparation for industrialized large-scale production to provide clinical needs. S...

Examples

Embodiment Construction

[0037] According to the above method, the following preparations of the present invention are prepared:

[0038] Formulation 1:

[0039] Etoposide or its pharmaceutically acceptable salt 50mg

[0040] Mannitol 150mg

[0041] Sodium bicarbonate amount

[0042] Formulation 2:

[0043] Etoposide or its pharmaceutically acceptable salt 100mg

[0044] Dextran 200mg

[0045] Sodium bicarbonate amount

[0046] Formulation 3:

[0047] Etoposide or its pharmaceutically acceptable salt 50mg

[0048] Glucose 200mg

[0049] Sodium bicarbonate amount

[0050] Formulation 4:

[0051] Etoposide or its pharmaceutically acceptable salt 50mg

[0052] Polyethylene Glycol 150mg

[0053] Sodium bicarbonate amount